KinasePro

Kinase Chemistry – Just a year and a half behind the times.

Archive for the ‘IKK’ Category

MLN-0415

Posted by kinasepro on May 2, 2009

Millenium’s beta-carboline’s aren’t new, but the structure of the Phase one IKK-B inhibitor hasn’t been released afaik.  Currrently in the Takeda pipeline via last years takeover.

ClC1=CC(NC([C@H]2N(CC(C)(OC2)C)CC(N3C[C@H](O[C@H](C3)C)C)=O)=O)=C(C4=C1)NC5=C4C=CN=C5WO/2009/054970

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Wyeth’s IKK candidate

Posted by kinasepro on October 23, 2008

US20080262010: D-glucuronate
US20080262009: acetate
US20080262008: succinate

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IKK-b or Jak?

Posted by kinasepro on June 4, 2007

So Merck’s got WO/2007/061764 and the wordplay makes me think the bit about JAK is just a diversion and that the primary target is IKK-b.  You have to squint a little to see the similarity with the Millennium series, but as usual: what do I know.  Interesting series none-the-less.

NC1=NC=C(C(N)=O)C2=C1C3=CC=C(C(F)(F)F)C=C3S2

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WO2007006926

Posted by kinasepro on January 25, 2007

Just another pyrimidine series? Maybe, but Sanofi-Aventis has a bunch of these sulfonamides in WO/2007/006926. They’ve got an IKK collaboration Millenium with “MLN0415 a phase one inhaled IKK-beta inhibitor taking the lead, but this aint that.

O=S(C1=CC=C(NC2=NC=CC(NC3=CC=C(F)C=C3)=N2)C=C1)(N(C4CCN(CCP(OCC)(OCC)=O)CC4)C[C@H]5CCCN5)=O

They’re not all phosphonates, but this subseries has me crooking an eyebrow. Perhaps this is the AVE8680 Sanofi series, but I’d expect this app to have Sxx# given that its a French application… eh… Beats me.

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US20060270671

Posted by kinasepro on December 4, 2006

Hi BI, nice IKK inhibitors. These seem to hav evolved from alcohol hits first published in that ’03 application, which led to these aminoalcohols (WO2005056562).

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